This data is provided as a convenience for informational purposes and to provide information about MRL Boston.

MARK T. GOULET, Ph.D.
Executive Director, Medicinal Chemistry

Goulet, M.T.; Mosley, R.T.  chapter:  “Peptidomimetics”, in Encyclopedia of Hormones, Academic Press, 2003.

Janovick JA, Goulet M, Bush E, Greer J, Wettlaufer DG, Conn PM.
Structure-activity relations of successful pharmacologic chaperones for rescue of naturally occurring and manufactured mutants of the gonadotropin-releasing hormone receptor. J Pharmacol Exp Ther. 2003 May;305(2):608-14.

Ujjainwalla F, Warner D, Walsh TF, Wyvratt MJ, Zhou C, Yang L, Kalyani RN, MacNeil T, Van der Ploeg LH, Rosenblum CI, Tang R, Vongs A, Weinberg DH, Goulet MT.
Design and syntheses of melanocortin subtype-4 receptor agonists: evolution of the pyridazinone archetype. Bioorg Med Chem Lett. 2003 Dec 15;13(24):4431-5.

Jiang J, DeVita RJ, Goulet MT, Wyvratt MJ, Lo JL, Ren N, Yudkovitz JB, Cui J, Yang YT, Cheng K, Rohrer SP.
Syntheses and structure-activity relationship studies of piperidine-substituted quinolones as nonpeptide gonadotropin releasing hormone antagonists. Bioorg Med Chem Lett. 2004 Apr 5;14(7):1795-8.

DeVita RJ, Parikh M, Jiang J, Fair JA, Young JR, Walsh TF, Goulet MT, Lo JL, Ren N, Yudkovitz JB, Cui J, Yang YT, Cheng K, Rohrer SP, Wyvratt MJ.
Identification of neutral 4-O-alkyl quinolone nonpeptide GnRH receptor antagonists. Bioorg Med Chem Lett. 2004 Nov 15;14(22):5599-603.

Ujjainwalla F, Warner D, Snedden C, Grisson RD, Walsh TF, Wyvratt MJ, Kalyani RN, Macneil T, Tang R, Weinberg DH, Van der Ploeg L, Goulet MT.
Design and syntheses of melanocortin subtype-4 receptor agonists. Part 2: Discovery of the dihydropyridazinone motif. Bioorg Med Chem Lett. 2005 Jul 6.

ILONA KARIV, Ph.D.
Director,Automated Lead Optimization

Wang MM, Schnabel CA, Chachisvilis M, Yang R, Paliotti MJ, Simons LA, McMullin L, Hagen N, Lykstad K, Tu E, Pestana LM, Sur S, Zhang H, Butler WF, Kariv I, Marchand PJ.
Optical forces for noninvasive cellular analysis. Appl Opt. 2003 Oct 1;42(28):5765-73.

Forster AH, Wang MM, Butler WF, Chachisvilis M, Chung TD, Esener SC, Hall JM, Kibar O, Lykstad K, Marchand PJ, Mercer EM, Pestana LM, Sur S, Tu E, Yang R, Zhang H, Kariv I.
Use of moving optical gradient fields for analysis of apoptotic cellular responses in a chronic myeloid leukemia cell model. Anal Biochem. 2004 Apr 1;327(1):14-22.

Wang MM, Tu E, Raymond DE, Yang JM, Zhang H, Hagen N, Dees B, Mercer EM, Forster AH, Kariv I, Marchand PJ, Butler WF.
Microfluidic sorting of mammalian cells by optical force switching. Nat Biotechnol. 2005 Jan;23(1):83-7.

NANCY E. KOHL, Ph.D.
Senior Director, Cancer Biology and Therapeutics

deSolms SJ, Ciccarone TM, MacTough SC, Shaw AW, Buser CA, Ellis-Hutchings M, Fernandes C, Hamilton KA, Huber HE, Kohl NE, Lobell RB, Robinson RG, Tsou NN, Walsh ES, Graham SL, Beese LS, Taylor JS.
Dual protein farnesyltransferase-geranylgeranyltransferase-I inhibitors as potential cancer chemotherapeutic agents. J Med Chem. 2003 Jul 3;46(14):2973-84.

Lobell RB, Davide JP, Kohl NE, Burns HD, Eng WS, Gibson RE.
A cell-based radioligand binding assay for farnesyl: protein transferase inhibitors.
J Biomol Screen. 2003 Aug;8(4):430-8.

Sepp-Lorenzino L, Rands E, Mao X, Connolly B, Shipman J, Antanavage J, Hill S, Davis L, Beck S, Rickert K, Coll K, Ciecko P, Fraley M, Hoffman W, Hartman G, Heimbrook D, Gibbs J, Kohl N, Thomas K.
A novel orally bioavailable inhibitor of kinase insert domain-containing receptor induces antiangiogenic effects and prevents tumor growth in vivo. Cancer Res. 2004 Jan 15;64(2):751-6.

Bilodeau MT, Balitza AE, Koester TJ, Manley PJ, Rodman LD, Buser-Doepner C, Coll KE, Fernandes C, Gibbs JB, Heimbrook DC, Huckle WR, Kohl N, Lynch JJ, Mao X, McFall RC, McLoughlin D, Miller-Stein CM, Rickert KW, Sepp-Lorenzino L, Shipman JM, Subramanian R, Thomas KA, Wong BK, Yu S, Hartman GD.
Potent N-(1,3-thiazol-2-yl)pyridin-2-amine vascular endothelial growth factor receptor tyrosine kinase inhibitors with excellent pharmacokinetics and low affinity for the hERG ion channel. J Med Chem. 2004 Dec 2;47(25):6363-72.

Hardwick JS, Yang Y, Zhang C, Shi B, McFall R, Koury EJ, Hill SL, Dai H, Wasserman R, Phillips RL, Weinstein EJ, Kohl NE, Severino ME, Lamb JR, Sepp-Lorenzino L.
Identification of biomarkers for tumor endothelial cell proliferation through gene expression profiling. Mol Cancer Ther. 2005 Mar;4(3):413-25.

Cox CD, Breslin MJ, Mariano BJ, Coleman PJ, Buser CA, Walsh ES, Hamilton K, Huber HE, Kohl NE, Torrent M, Yan Y, Kuo LC, Hartman GD.
Kinesin spindle protein (KSP) inhibitors. Part 1: the discovery of 3,5-diaryl-4,5-dihydropyrazoles as potent and selective inhibitors of the mitotic kinesin KSP. Bioorg Med Chem Lett. 2005 Apr 15;15(8):2041-5.

Tao W, South VJ, Zhang Y, Davide JP, Farrell L, Kohl NE, Sepp-Lorenzino L, Lobell RB.
Induction of apoptosis by an inhibitor of the mitotic kinesin KSP requires both activation of the spindle assembly checkpoint and mitotic slippage. Cancer Cell. 2005 Jul;8(1):49-59.